ChemicalBook > CAS DataBase List > PF-543 (Citrate)

PF-543 (Citrate)

Product Name: PF-543 (Citrate)
CAS No.: 1415562-83-2
Chemical Name: PF-543 (Citrate)
Synonyms: PF-543 (Citrate);PWXXWUWKNPXSGW-VQIWEWKSSA-N;PF543 CITRATE; PF 543 CITRATE;Sphingosine Kinase 1 Inhibitor II Citrate;(2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol 2-hydroxy-1,2,3-propanetricarboxylate;(2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
CBNumber: CB12645149
Molecular Formula: C33H39NO11S
Formula Weight: 657.73
MOL File: 1415562-83-2.mol

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PF-543 (Citrate) Property

form: Powder
color: White to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-1072
Product name: PF-543(Citrate)
Purity: 98.10%
Packaging: 5mg
Price: $95
Updated: 2021/12/16

Axon Medchem

Product number: Axon2350
Product name: PF543citrate
Purity: 98%
Packaging: 5mg
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Updated: 2021/12/16

ApexBio Technology

Product number: A3718
Product name: PF-543Citrate
Packaging: 5mg
Price: $110
Updated: 2021/12/16

ChemScene

Product number: CS-1072
Product name: PF-543(Citrate)
Purity: 98.10%
Packaging: 10mg
Price: $140
Updated: 2021/12/16

ApexBio Technology

Product number: A3718
Product name: PF-543Citrate
Packaging: 10mg
Price: $195
Updated: 2021/12/16

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PF-543 (Citrate) Chemical Properties,Usage,Production

Uses

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy[1][2][3].

in vivo

PF-543 (1 mg/kg; intraperitoneal injection; every second day; for 21 days; female C57BL/6 J mice) treatment has no effect on vascular remodelling but reduces right ventricular hypertrophy. The protection involves a reduction in the expression of p53 and an increase in the expression of anti-oxidant nuclear factor Nrf-2^[2].
? Mice are initially dosed (ip) with 10 mg/kg or 30 mg/kg of PF-543 for 24 h and the T_1/2 is 1.2 h in blood samples. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels^[2].

Animal Model:	Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension^[2]
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; every second day; for 21 days
Result:	Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2.

IC 50

SphK1

References

[1] Schnute ME, et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012 May 15;444(1):79-88. DOI:10.1042/BJ20111929
[2] MacRitchie N, et al. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension. Cell Signal. 2016 Aug;28(8):946-55. DOI:10.1016/j.cellsig.2016.03.014
[3] Hamada M, et al. Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells. Cell Death Discov. 2017 Aug 14;3:17047. DOI:10.1038/cddiscovery.2017.47

PF-543 (Citrate) Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-543 (Citrate) Suppliers

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PF-543 (Citrate)

(2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol 2-hydroxy-1,2,3-propanetricarboxylate (1:1)

(2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol 2-hydroxy-1,2,3-propanetricarboxylate

PWXXWUWKNPXSGW-VQIWEWKSSA-N

PF543 CITRATE; PF 543 CITRATE

Sphingosine Kinase 1 Inhibitor II Citrate

1415562-83-2

C33H39NO11S

C6H8O7C27H31NO4S

C27H31NO4SC6H8O7